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2-Bromopropane → N-[1-(3,5-Diisopropoxy-benzyl)-piperidin-4-yl]-2,6-dimethyl-terephthalamic acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-Bromopropane | HCID 6358 | — |
| 反応物 | Trifluoroacetic acid | HCID 6422 | — |
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | 3,5-Dihydroxybenzaldehyde | HCID 94365 | — |
| 反応物 | Sodium cyanoborohydride | HCID 5003444 | — |
| 反応物 | 3,5-diisopropoxybenzaldehyde | HCID 11310605 | — |
| 反応物 | 2,6-dimethyl-N-piperidin-4-yl-terephthalamic acid | HCID 68456914 | — |
| 反応物 | 4-(4-Tert-butoxycarbonyl-3,5-dimethyl-benzoylamino)-piperidine-1-carboxylic acid tert-butyl ester | HCID 68459100 | — |
| 溶媒 | Acetic Acid | HCID 176 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | N-[1-(3,5-Diisopropoxy-benzyl)-piperidin-4-yl]-2,6-dimethyl-terephthalamic acid | HCID 68454639 | — |
反応手順
In analogy to the procedure described in example 50k), 2,6-dimethyl-N-piperidin-4-yl-terephthalamic acid [prepared from 4-(4-tert-butoxycarbonyl-3,5-dimethyl-benzoylamino)-piperidine-1-carboxylic acid tert-butyl ester and trifluoroacetic acid in dichloromethane in analogy to the procedure described in example 50i)] was reacted with 3,5-diisopropoxy-benzaldehyde [prepared from 3,5-dihydroxy-benzaldehyde and 2-bromopropane, potassium carbonate in DMF at 60° C. in analogy to the procedure described in example 50e)], sodium cyanoborohydride, N-ethyl-diisopropylamine and acetic acid in ethanol at 50° C. to yield the title compound as light yellow solid. MS: 483.3 (MH+).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07772253B2 |
| 出典データセット | uspto-grants-2010_08 |
| ORD ID | ord-ab22671dc0ac441f929df473d29d604d |
| 出典メモ | uspto-grants-2010_08 |